IC261 [Ligand Id: 5985] activity data from GtoPdb and ChEMBL
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| ChEMBL ligand: CHEMBL576349 (IC261) |
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| DB | Assay description | Assay Type | Standard value | Standard parameter | Original value | Original units | Original parameter | Reference |
|---|---|---|---|---|---|---|---|---|
| casein kinase 1 alpha 1/Casein kinase I alpha in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2793] [GtoPdb: 1995] [UniProtKB: P48729] | ||||||||
| GtoPdb | - | - | 4.8 | pIC50 | 16000 | nM | IC50 | J Biol Chem (2000) 275: 20052-60 [PMID:10749871] |
| ChEMBL | Inhibition of CK1alpha | B | 5.91 | pIC50 | 1240 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5672-5675 [PMID:18799313] |
| ChEMBL | Inhibition of CK1 using KRRRALS(p)VASLPGL as substrate after 40 mins by scintillation counter | B | 6 | pIC50 | 1000 | nM | IC50 | Eur J Med Chem (2012) 56: 30-38 [PMID:22944772] |
| casein kinase 1 delta/Casein kinase I delta in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2828] [GtoPdb: 1997] [UniProtKB: P48730] | ||||||||
| ChEMBL | Inhibition of CK1delta | B | 5.59 | pIC50 | 2570 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5672-5675 [PMID:18799313] |
| ChEMBL | Inhibition of human CK1delta expressed in simian genome expressing mouse 3T3 cells | B | 5.59 | pIC50 | 2570 | nM | IC50 | Bioorg Med Chem Lett (2010) 20: 2958-2963 [PMID:20350806] |
| GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 | J Biol Chem (2000) 275: 20052-60 [PMID:10749871] |
| ChEMBL | Inhibition of human CK1delta | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2009) 52: 7618-7630 [PMID:19591487] |
| ChEMBL | Inhibition of human recombinant CK-1delta using casein as substrate after 60 mins by Kinase-Glo assay | B | 6 | pIC50 | 1000 | nM | IC50 | J Med Chem (2014) 57: 2755-2772 [PMID:24592867] |
| casein kinase 1 gamma 1/Casein kinase I gamma 1 in Human (target type: SINGLE PROTEIN) [ChEMBL: CHEMBL2426] [GtoPdb: 1999] [UniProtKB: Q9HCP0] | ||||||||
| ChEMBL | Inhibition of CK1gamma1 | B | 4.4 | pIC50 | >40000 | nM | IC50 | Bioorg Med Chem Lett (2008) 18: 5672-5675 [PMID:18799313] |
| Plasmodium falciparum (target type: ORGANISM) [ChEMBL: CHEMBL364] | ||||||||
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum GB4 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum HB3 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum W2 after 72 hrs by SYBR green assay | F | 4.9 | pIC50 | 12589.25 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| ChEMBL | Antiplasmodial activity against Plasmodium falciparum 7G8 after 72 hrs by SYBR green assay | F | 5 | pIC50 | 10000 | nM | IC50 | Nat Chem Biol (2009) 5: 765-771 [PMID:19734910] |
| casein kinase 1 epsilon in Human [GtoPdb: 1998] [UniProtKB: P49674] | ||||||||
| GtoPdb | - | - | 6 | pIC50 | 1000 | nM | IC50 | J Biol Chem (2000) 275: 20052-60 [PMID:10749871] |
ChEMBL data shown on this page come from version 34:
Zdrazil B, Felix E, Hunter F, Manners EJ, Blackshaw J, Corbett S, de Veij M, Ioannidis H, Lopez DM, Mosquera JF, Magarinos MP, Bosc N, Arcila R, Kizilören T, Gaulton A, Bento AP, Adasme MF, Monecke P, Landrum GA, Leach AR. (2024). The ChEMBL Database in 2023: a drug discovery platform spanning multiple bioactivity data types and time periods. Nucleic Acids Res., 52(D1). DOI: 10.1093/nar/gkad1004. [EPMCID:10767899] [PMID:37933841]
Davies M, Nowotka M, Papadatos G, Dedman N, Gaulton A, Atkinson F, Bellis L, Overington JP. (2015) 'ChEMBL web services: streamlining access to drug discovery data and utilities.' Nucleic Acids Res., 43(W1). DOI: 10.1093/nar/gkv352. [EPMCID:25883136]
